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Application of phenylpropanoid glycosides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors

A technology of phenylpropanoid glycosides and compounds, applied in the direction of drug combinations, medical preparations containing active ingredients, antibacterial drugs, etc.

Active Publication Date: 2018-11-13
江苏凯吉生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] For this reason, the technical problem to be solved in the present invention is the problem that no phenylpropanoid glycosides are used for the preparation of IDO inhibitors in the prior art, thereby providing the purposes of phenylpropanoid glycosides in the preparation of IDO inhibitors

Method used

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  • Application of phenylpropanoid glycosides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors
  • Application of phenylpropanoid glycosides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors
  • Application of phenylpropanoid glycosides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Preparation of Verascoside and Cistanche glycoside D

[0033] Take the dried succulent stems of Cistanche deserticola Ma, add 10 times the weight of the 75% ethanol aqueous solution by heating and reflux for extraction twice, the first extraction is 2 hours, the second extraction is 1 hour, the extracts are combined, and the Press and concentrate to obtain Cistanche deserticola extract;

[0034] Suspended the Cistanche deserticola extract in 1 times the weight of water, then extracted twice with n-butanol as the extractant, collected the organic phase of the extract, and concentrated under reduced pressure to obtain the extract of the n-butanol extraction part of Cistanche deserticola;

[0035] The n-butanol extract of Cistanche deserticola was purified by AB-8 macroporous resin column chromatography (the diameter of the macroporous resin column was 8 cm, and the column volume was 3.5 L), using water as mobile phase A and ethanol as mobile phase B , and carr...

experiment example 1

[0039] Experimental example 1 Inhibitory Activity of Verbasin and Cistanche D on IDO

[0040] 1. The purpose of the experiment

[0041] HEK293 cells were transfected with plasmid pcDNA3.1-IDO to make it highly express IDO, and then the inhibitory activities of verbascoside and cistanoside D on IDO at the cellular level were determined respectively.

[0042] 2. Experimental method

[0043] HEK 293 cells were seeded in a 96-well plate at a density of 2.5×104 cells / well, cultured in DMEM medium (containing 10% fetal bovine serum, 50U / mL penicillin and 50mg / mL streptomycin), placed at 37°C, humidity 95%, 5% CO 2 cultured in an incubator. After culturing for 24 hours, liposome Lipofectamin 2000 was used to mediate pcDNA3.1-hIDO plasmid transfection, and they were divided into positive control group and experimental group 1-2. The positive control group used 1-methyltryptophan (1-MT) as the test product, and the experimental groups 1-2 used the verbascoside and cistanoside D p...

experiment example 2

[0053] Experimental example 2 Therapeutic effect of phenylpropanoid glycosides on ankylosing spondylitis

[0054] 1. The purpose of the experiment

[0055] The mouse model of ankylosing spondylitis was established by proteoglycan immunization, and then the verascoside and Cistanche D were administered orally. The serum levels of inflammatory markers TNF-α and NF-κB receptor activator ligand (RANKL) were detected by ELISA. , and detected serum IDO activity (Kyn / Trp) to verify the efficacy of phenylpropanoid glycosides for ankylosing spondylitis.

[0056] 2. Experimental method

[0057] 2.1 Experimental animals

[0058] Thirty-two healthy male BALB / c mice, weighing (18±2) g, aged 4-5 weeks, were purchased from Shanghai Slack.

[0059] 2.2 Test drugs

[0060] Verbasin and Cistanche glycoside D prepared in Example 1 were used as test drugs.

[0061] 2.3 Experiment grouping and modeling

[0062] After 1 week of adaptive feeding of mice, 8 of them were taken as blank control...

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Abstract

The invention belongs to the field of medicines or health products and particularly relates to phenylpropanoid glycosides and application of their pharmaceutically-acceptable derivatives in the preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors. Researches herein discover that both acteoside and cistanoside D have better inhibitory activity against IDO in cells than that of 1-MT (1-methyl-tryptophan) against IDO in cells, have significant IDO inhibitory activity, and are suitable for treating cancers, Alzheimer's disease, ankylosing spondylitis, autoimmune diseases, bacterial infections, cataract, mood disorders, and depression or anxiety.

Description

technical field [0001] The invention belongs to the field of medicines or health products, and in particular relates to the use of phenylpropanoid glycosides in the preparation of IDO inhibitors. Background technique [0002] IDO (indoleamine-2,3-dioxygenase) is the only rate-limiting enzyme outside the liver that catalyzes the metabolism of tryptophan along the kynurenine pathway (KP). , tryptophan can be decomposed into various metabolites such as L-kynurenine, picolinic acid and quinolinic acid. L-tryptophan is an essential amino acid for maintaining cell activation and proliferation in the human body, and it is also an indispensable component of protein. L-tryptophan can lead to abnormal functions of some important cells. Since its discovery in 1967, the mechanism by which IDO inhibits the proliferation of pathogenic microorganisms by degrading tryptophan, and the relationship between IDO and neurological diseases have gradually been elucidated; and studies have confirm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7032A61P35/00A61P25/28A61P19/08A61P37/02A61P31/04A61P27/12A61P25/22A61P25/24A61P25/00
CPCA61K31/7032
Inventor 温尧林
Owner 江苏凯吉生物科技有限公司
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